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Assay Detail

CHEMBL4730611

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bcl-2-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X Inhibitor.
Wang L,Doherty GA,Judd AS,Tao ZF,Hansen TM,Frey RR,Song X,Bruncko M,Kunzer AR,Wang X,Wendt MD,Flygare JA,Catron ND,Judge RA,Park CH,Shekhar S,Phillips DC,Nimmer P,Smith ML,Tahir SK,Xiao Y,Xue J,Zhang H,Le PN,Mitten MJ,Boghaert ER,Gao W,Kovar P,Choo EF,Diaz D,Fairbrother WJ,Elmore SW,Sampath D,Leverson JD,Souers AJ
ACS Med Chem Lett (2020) 11 : 1829 -1836
PubMed 33062160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.76 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935328 1 10.57
CHEMBL3891330 1 10.36
CHEMBL3972984 1 9.53
CHEMBL3901568 1 9.48
CHEMBL3912857 1 9.19
CHEMBL3910958 1 8.30
CHEMBL3983880 1 8.22
CHEMBL3287296 1 7.96
CHEMBL3287293 1 7.19
CHEMBL3287292 1 6.79
CHEMBL3919588 1 -
CHEMBL3793424 1 -
CHEMBL4762875 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935328 Ki = 0.027 nM 10.57
CHEMBL3891330 Ki = 0.044 nM 10.36
CHEMBL3972984 Ki = 0.296 nM 9.53
CHEMBL3901568 Ki = 0.329 nM 9.48
CHEMBL3912857 Ki = 0.65 nM 9.19
CHEMBL3910958 Ki = 5.0 nM 8.30
CHEMBL3983880 Ki = 5.96 nM 8.22
CHEMBL3287296 Ki = 11.0 nM 7.96
CHEMBL3287293 Ki = 65.0 nM 7.19
CHEMBL3287292 Ki = 164.0 nM 6.79
CHEMBL3919588 Ki = 0.008 nM -
CHEMBL3793424 Ki < 0.01 nM -
CHEMBL4762875 Ki < 0.01 nM -